This invention relates to novel antibiotics, phosphonic acid derivatives which have antimicrobial activities against various pathogenic bacteria, to processes for production thereof, and to pharmaceutical compositions comprising the same.
The inventors of this invention first and originally isolated a new antibiotic, hereinafter called the antibiotic FR-900098, in pure form from a cultured broth obtained by fermentation of a strain of genus Streptomyces, identified the same by the physico-chemical properties and also discovered the utility thereof, namely that said antibiotic FR-900098 has antimicrobial activities against various pathogenic microorganisms.
After the first isolation of the antibiotic FR-900098, said antibiotic FR-900098 was delivered to the chemists (i.e. the inventors of U.S. application Ser. No. 819,554 filed on the same date as the filing date of this application) of the Synthesis section of the Research Laboratory of Fujisawa Pharmaceutical Co., Ltd., Japan to which the inventors of this invention also belonged, for identification of its chemical structure. Then, said chemists succeeded in identifying the chemical structure and assigned the chemical structure to the antibiotic FR-900098 as follows. ##STR3## [3-(N-acetyl-N-hydroxyamino)propylphosphonic acid] Further, the inventors of this invention first and originally isolated another antibiotic, hereinafter called the antibiotic FR-33289 from a cultured broth obtained by fermentation of a strain of genus Streptomyces, identified the same by the physico-chemical properties and the chemical structure which is assigned as follows, and discovered the utility thereof, namely that said antibiotic FR-33289 has antimicrobial activities against various pathogenic microorganisms. ##STR4## [3-(N-acetyl-N-hydroxyamino)-2-hydroxypropylphosphonic acid]
With regard to the novel antibiotics mentioned above, it is to be noted that the chemists indicated above made extensive studies on synthetic methods for preparing the same and succeeded in devising synthetic methods for preparing the antibiotic FR-900098 as well as the antibiotic FR-33289, including various derivatives thereof, which was filed as a U.S. patent application under the Ser. No. 819,554 on the same date as the filing date of this U.S. patent application.